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Synthesis 2010(21): 3700-3704  
DOI: 10.1055/s-0030-1258269
PAPER
© Georg Thieme Verlag Stuttgart ˙ New York

A New and Improved Synthesis of the Precursor of the Hypoxia Marker [¹8F]-FMISO

Elena Nietoa, Ramón Alajarína, Julio Álvarez-Builla*a, Ignacio Larrañagab, Elena Gorospeb, Miguel A. Pozoc
a Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Alcalá, Ctra. Madrid-Barcelona km 33.6, 28871 Alcalá de Henares, Madrid, Spain
Fax: +34918854686; e-Mail: julio.alvarez@uah.es;
b Instituto Tecnológico PET, Manuel Bartolomé Cossío, 28040 Madrid, Spain
c Instituto Pluridisciplinar, Universidad Complutense de Madrid, Paseo Juan XXIII, 28040 Madrid, Spain
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Publikationsverlauf

Received 23 June 2010
Publikationsdatum:
28. September 2010 (online)

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Abstract

A new synthetic approach to the precursor of the hypoxia marker [¹8F]-FMISO has been developed. Three different tosylation methods were studied for the preparation of the key intermediate. The overall yield is markedly higher than the yields reported for previous syntheses. The precursor was used to prepare [¹8F]-FMISO and the results were comparable to those obtained when a commercial precursor was used.

Key words

[¹8F]-FMISO - hypoxia - radiopharmaceutical - regioselective tosylation

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